GABA R

GABA (r-aminobutyric acid) May have presynaptic effects on excitatory ENS nerve terminals. Has some relaxant effect on the gut. Probably not a major transmitter in the ENS. 

Laudanosine (= Laudanine Papaver somniferum (opium poppy) GABA-R antagonist (100)... 

Anisatin Illicium anisatum (Japanese star anise) GABA-R non-competitive... 

Ginsenoside Rg2 Panax ginseng (Araliaceae) [root] GABA-R antagonist... 

Gly-R ligand (effect reversed by Gly-R antagonist Strychnine) (GABA-R) [neurotoxic]... 

Succinic semialdehyde (SSA) is synthesized in the mitochondria through transamination of y-aminobutyric acid (GABA) by GABA transaminase (GABA-T). Most of the SSA is oxidized by SSA dehydrogenase (SSA-DH) to form succinate, which is used for energy metabolism and results in the end products CO2 + H2O, which are expired. A small portion of SSA (<2%) is converted by SSA reductase (SSA-R) in the cytosol to GHB. GHB may also be oxidized back to SSA by GHB dehydrogenase (GHB-DH). 

Von Keyserlingk, H.C. and Willis, R.J. (1992). The GABA-activated CL channel in insects as a target for insecticide action—a physiological study. In D. Otto and B. Weber (Eds.) Insecticides Mechanism of Action and Resistance. Andover, U.K. Intercept. 

Cotter R, Williams C, Ryan L et al (2002) FractaUdne (CX3CL1) and brain inflammation impU-cations for HIV-l-associated dementia. J Neurovirol 8 585-598 Cunha-Reis D, Ribeiro JA, Sebastiao AM (2008) Al and A2A receptor activation by endogenous adenosine is required for VIP enhancement of K+-evoked [3H]-GABA release from rat hippocampal nerve terminals. Neurosci Lett 430 207-212 Davalos D, Grutzendler J, Yang G et al (2005) ATP mediates rapid microglial response to local brain injury in vivo. Nat Neurosci 8 752-758... 

Roberts, E (1986) GABA the road to neurotransmitter status. In BenzodiazepinejGABA receptors and chloride channels structural and functional properties (Eds Olsen, R and Venter, CJ), Alan R. Liss, New York, pp. 1-39. 

Fig. 5.12 (a) Synaptic types along dendritic spines of M/T and GC units uni-, and bi-directional junctions, (b) Transmitter systems at a reciprocal synapse, Mitral-Granule cell junction. [Glu, glutamate (R, receptor) GABA, y-aminobutyric acid (R, receptor) E, intracellular effector and aAR, alpha-adrenergic receptor.]. (From Hayashi et al., 1993.)... 

Serretti, A., Lilli, R., Lorenzi, C. etal. (1999). Dopamine receptor D2 and D4 genes, GABA(A) alpha-1 subunit genes and response to lithium prophylaxis in mood disorders. Psychiatry Res., 87, 7-19. 

Harris-Warrick R. (2005). Synaptic chemistry in single neurons GABA is identified as an inhibitory neurotransmitter. J. Neurophysiol. 93, 3029-31. 

Lee, R. S., Steffensen, S. C. Henriksen, S. J. (2001). Discharge profiles of ventral tegmental area GABA neurons during movement, anesthesia, and the sleep-wake cycle. J. Neurosci. 21, 1757-66. 

Kaur, S., Saxena, R. N. Malhck, B. N. (1997). GABA in locus coeruleus regulates spontaneous rapid eye movement sleep by acting on GABAA receptors in freely moving rats. Neurosci. Lett. 223, 105-8. 

Liu, R., Jolas, T. Aghajanian, G. (2000). Serotonin 5-HT(2) receptors activate local GABA inhibitory inputs to serotonergic neurons of the dorsal raphe nucleus. Brain Res. 873, 34-45. 

Pollock, M. S. Mistlberger, R. E. (2003). Rapid eye movement sleep induction by microinjection of the GABA-A antagonist bicuculline into the dorsal subcoeruleus area of the rat. Brain Res. 962, 68-77. 

Baumann, S. W., Baur, R. 8r Sigel, E. (2003). Individual properties of the two functional agonist sites in GABA(A) receptors./. Neurosci. 23, 11158-66. 

Epperson, C.N.O.M.S., Czarkowski, K.A., Gueorguieva, R., Jatlow, R, Sanacora, G., Rothman, D.L., Krystal, J.H., Mason, G.F. Sex, GABA, and nicotine the impact of smoking on cortical GABA levels across the menstrual cycle as measured with proton magnetic resonance. Biol. Psychiatry. 57 44, 2005. 

Stromberg M.F., Mackler S.A., Volpicelli J.R., O Brien C.P., Dewey S.L. The effect of gamma-vinyl-GABA on the consumption of concurrently available oral cocaine and ethanol in the rat. Pharmacol. 

Brebner K., Childress A.R., Roberts D.C. A potential role for GABA(B) agonists in the treatment of psychostimulant addiction. Alcohol Alcohol. 37 478, 2002. 

Winkler, M., Knall, A.C., Kulterer, M.R. and Klempier, N. (2007) Nitrilases catalyze key step to conformationally constrained GABA analogous y-amino acids in high optical purity. The Journal of Organic Chemistry, 72, 7423-7426. 

Imidazopyridothiazines (and imidazopyridopyrazines) can be prepared from the corresponding aminochloropyr-idines in a one-pot reaction, as shown in Scheme 69. Products in which R= l,2,4-oxadiazol-3-yl are of interest as possible 7-aminobutyric acid (GABA) receptor ligands <2002M653, 2002M1205>. 

Sachs, M. S., Wang, Z., Gaba, A., Fang, P., Belk, J., Ganesan, R., Amrani, N., and Jacobson, A. (2002). Toeprint analysis of the positioning of translation apparatus components at initiation and termination codons of fungal mRNAs. Methods 26, 105-114. 

A similar pathway involving a microwave-driven molybdenum-catalyzed asymmetric allylic alkylation as the key step was elaborated by Moberg and coworkers for the preparation of the muscle relaxant (R)-baclofen (Scheme 6.52) [108]. The racemic form of baclofen is used as a muscle relaxant (antispasmodic) lipophilic derivative of y-aminobutyric acid (GABA). Pharmacological studies have shown that the (R)-enantiomer is the therapeutically useful agonist of the GABAb receptor. Asymmetric alkylation of the allylic carbonate precursor with dimethyl malonate afforded... 

Behar KL, Rothman DL, Petersen KF, Hooten M, Delaney R, Petroff OA, Shulman GI, Navarro V, Petrakis IL, Chamey DS, Krystal JH Preliminary evidence of low cortical GABA levels in localized 111-MR spectra of alcohol-dependent and hepatic encephalopathy patients. Am J Psychiatry 1999 156 952-954. 

Avallone R, Zanoli P, Corsi L, Cannazza G, Baraldi M Benzodiazepine-like compounds and GABA in flower heads of Matricaria cha-momilla. PhytotherRes 1996 10 177-179. 

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